METHOD FOR PRODUCTION OF HYDROXYLATED CYCLOPENTYL PYRIMIDINE COMPOUNDS Russian patent published in 2018 - IPC C07D403/04 C07D239/28 

FIELD: pharmacology.

SUBSTANCE: compounds of formula I can be used to prepare compounds possessing the properties of an ACT kinase inhibitor for treatment of diseases such as cancer. The method for preparation of a compound of formula I comprises cyclising of a compound of formula II or a salt thereof, wherein R¹ is t-butoxycarbonyl; R² is -COOR^a, where R^a is hydrogen or unsubstituted C_1-4 alkyl, or R² is-CONR^aR^b, where R^a is unsubstituted C_1-4 alkyl and R^b is -OR^c, phenyl; or R^a and R^b are taken together with the atom to which they are attached to form a 5-7 membered heterocyclyl, further comprising an oxygen atom; R^c is C_1-4 alkyl; and M is Li or Mg. At that, a compound of formula II or a salt thereof obtained by contacting of a compound of formula III or a salt thereof, wherein R³ is bromine or iodine, with a magnesium or lithium metal-containing agent, for example alkyl magnesium halide, is used. The compound of formula III is usually prepared by reacting a compound of formula IV or a salt thereof with compound to produce a compound of formula V or a salt thereof, wherein R⁴ is -Cl or -OH, R¹ and R² have the values indicated above. The invention also relates to new intermediates, a compound of formula III and a compound of formula IV.

EFFECT: method allows to obtain products on an industrial scale with comparable or increased yield and quality of products.

22 cl, 1 tbl, 6 ex

,